- An Activity-Based Sensing Fluorogenic Probe for Monitoring Ethylene in Living Cells and Plants
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Ethylene (ET) is an important gaseous plant hormone. It is highly desirable to develop fluorescent probes for monitoring ethylene in living cells. We report an efficient RhIII-catalysed coupling of N-phenoxyacetamides to ethylene in the presenc
- Chen, Yiliang,Guo, Duojing,Jing, Maofeng,Li, Ji,Li, Yu,Liu, Hao,Wang, Biao,Wei, Lirong,Yan, Wei,Ye, Yonghao,Yu, Na,Zhao, Jing,Zheng, Ying
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supporting information
p. 21934 - 21942
(2021/08/30)
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- Fluorous tagged N-hydroxy phthalimide for the parallel synthesis of O-aryloxyamines
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The parallel synthesis of O-aryloxyamines remains an unfulfilled need in the field of medicinal chemistry and fragment-based approaches. To fill this gap a solution-phase two-step process based on (1) a copper-catalyzed cross-coupling of aryl boronic acid
- Gaucher-Wieczorek, Florence S.,Maillard, Ludovic T.,Badet, Bernard,Durand, Philippe
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scheme or table
p. 655 - 658
(2010/10/21)
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- Inhibitors of transthyretin amyloid fibril formation
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Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.
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Page/Page column 9; sheet 6
(2008/06/13)
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- Bisaryloxime ethers as potent inhibitors of transthyretin amyloid fibril formation
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Amyloid fibril formation by the plasma protein transthyretin (TTR), requiring rate-limiting tetramer dissociation and monomer misfolding, is implicated in several human diseases. Amyloidogenesis can be inhibited through native state stabilization, mediated by small molecule binding to TTR's primarily unoccupied thyroid hormone binding sites. New native state stabilizers have been discovered herein by the facile condensation of arylaldehydes with aryloxyamines affording a bisarylaldoxime ether library. Of the library's 95 compounds, 31 were active inhibitors of TTR amyloid formation in vitro. The bisaryloxime ethers selectively stabilize the native tetrameric state of TTR over the dissociative transition state under amyloidogenic conditions, leading to an increase in the dissociation activation barrier. Several bisaryloxime ethers bind selectively to TTR in human blood plasma over the plethora of other plasma proteins, a necessary attribute for efficacy in vivo. While bisarylaldoxime ethers are susceptible to degradation by N-O bond cleavage, this process is slowed by their binding to TTR. Furthermore, the degradation rate of many of the bisarylaldoxime ethers is slow relative to the half-life of plasma TTR. The bisaryloxime ether library provides valuable structure-activity relationship insight for the development of structurally analogous inhibitors with superior stability profiles, should that prove necessary.
- Johnson, Steven M.,Petrassi, H. Michael,Palaninathan, Satheesh K.,Mohamedmohaideen, Nilofar N.,Purkey, Hans E.,Nichols, Christopher,Chiang, Kyle P.,Walkup, Traci,Sacchettini, James C.,Sharpless, K. Barry,Kelly, Jeffery W.
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p. 1576 - 1587
(2007/10/03)
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- Synthesis and opioid activities of some naltrexone oxime ethers
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A series of alkyl, cycloalkyl, aryl, and aralkyl ethers of naltrexone oxime was prepared.The compounds were examined in binding assays for μ, δ, and κ opioid receptor affinity.In addition, the naltrexone oxime ethers were studied in animal models that measure opioid agonist and antagonist activity.These studies led to the discovery of several compounds, notably phenethyl 3e and phenylpropyl 3f ethers of naltrexone, which have a 10-fold increase in potency at the κ opioid receptor with potent μ and κ agonist properties in vivo.naltrexone / oxime ether / opioid receptor / analgesia / receptor binding / kappa
- Mavunkel, B. J.,Rzeszotarski, W. J.,Kaplita, P. V.,DeHaven-Hudkins, D. L.
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p. 659 - 666
(2007/10/02)
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